Hello Bio/SR 95531 hydrobromide (Gabazine)/HB0901/10mM (add 1ml water)

Product overview

• Name
  SR 95531 hydrobromide (Gabazine)
• Short description
  Selective, competitive GABA_A receptor antagonist
• Biological description

  Selective and competitive GABA_A receptor antagonist (K_i = 150 nM for displacement of [³H]-GABA from rat membranes).

  
  Displaces GABA from the GABA_AR agonist binding site to prevent receptor activation. Also acts as a negative allosteric inhibitor of channel opening to inhibit GABA_A receptor activation by anaesthetic agents.

  
  Inhibits GABA-induced Cl- currents to reduce GABA-mediated synaptic inhibition.

  
  Also displays low affinity glycine receptor inhibition.

  
  Shows convulsive actions.

• Alternative names
  Gabazine | GBZ
• Biological action
  Antagonist
• Purity
  >98%
• Customer comments

  We regularly use Hello Bio Gabazine (SR 95531) in the lab.We especially like the formulation where you only need to add 1ml of water to make a 10mM stock solution. Verified customer, The University of Newcastle

  I am satisfied with the quality, quick delivery and follow-up of your product. Verified customer, Shimane University

  We used our first aliquot of SR95531 (Gabazine) last week. The experiment was a critical one for us and the SR95531 worked exactly as expected – 100% block of a GABAergic IPSP (inhibitory postsynaptic potential). Verified customer, University of Michigan

• Our products in action
  5 citationsSubmit Your Citation Now

Images

Properties

• Chemical name
  6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
• Molecular Weight
  368.23
• Chemical structure
  
• Molecular Formula
  C₁₅H₁₇N₃O₃.HBr
• CAS Number
  104104-50-9
• PubChem identifier
  107895
• SMILES
  COC1=CC=C(C=C1)C2=NN(C(=N)C=C2)CCCC(=O)O.Br
• Source
  Synthetic
• InChi
  InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
• InChiKey
  GFZHNFOGCMEYTA-UHFFFAOYSA-N
• MDL number
  MFCD00055135
• Appearance
  White solid

Applications

• Application notes

  Gabazine (SR 95531) is commonly used to reduce levels of inhibition by antagonising GABA_A receptors. It is commonly used at concentrations between 10 – 200 μM.

  Gabazine (SR 95531) from Hello Bio blocks spontaneous inhibitory post synaptic currents (IPSC) and evoked IPSCs (see Fig 1 above). It was effective at 1 μM and completely blocked GABA_A receptors at 20 μM.

   

  #Protocol 1: Evoked and spontaneous inhibitory post synaptic currents (IPSCs)

  • Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
  • A stimulating electrode was placed in layers II/III and IPSCs were evoked by a single square (150 μs) pulse every 10 sec at a stimulus intensity that gave a reliable IPSC.
  • IPSCs were evoked at a range of neuron holding voltages to measure the reversal potential of the current to ensure it was GABAergic.
  • Neurons were held at 0mV and IPSCs continuously stimulated and recorded in response to 5 min applications of varying concentrations of Gabazine until complete receptor inhibition.
  • Spontaneous IPSCs were recorded before and after addition of Gabazine by holding the neuron at 0mV and recording for 10 sec.
  • All recordings for IPSCs were made in the presence of AMPAR antagonists.

Storing and Using Your Product

• Storage instructions
  Room temperature
• Solubility overview
  Soluble in water (25mM) and in DMSO (100mM)
• Important
  This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.